ZINC69391
目录号: PL10883 纯度: ≥99%
CAS No. :303094-67-9
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中文名称
ZINC69391
英文名称
ZINC69391
英文别名
2-(4,6-dimethylpyrimidin-2-yl)-1-[2-(trifluoromethyl)phenyl]guanidine;N'-(4,6-dimethylpyrimidin-2-yl)-N-[2-(trifluoromethyl)phenyl]guanidine;N-(4,6-Dimethyl-2-pyrimidinyl)-N'-[2-(trifluoromethyl)phenyl]-guanidine;SMSF0013930;CB12619;Z56785930;ZINC69391
Cas No.
303094-67-9
分子式
C14H14F3N5
分子量
309.29
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
ZINC69391 是一种特异的 Rac1 抑制剂,通过在 Rac1 表面掩蔽 Trp56 残基来干扰 Rac1-GEF 的相互作用。ZINC69391 干扰 Rac1 与 Dock180 的相互作用,降低 Rac1-GTP水平。ZINC69391 诱导细胞凋亡,具有抗增殖和抗转移作用。
生物活性
ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects.
性状
Solid
体外研究(In Vitro)
ZINC69391 inhibits growth of U937, HL-60, KG1A and Jurkat cells with IC50s ranging from 41 to 54 μM.
ZINC69391 (50-100 μM; 24 hours) augments the enzymatic activity of caspase 3 in a concentration dependent manner.
ZINC69391 (0-125 μM; 72h) reduces cell proliferation of human glioma cells.
ZINC69391 (50-100 μM; 48 hours) triggers cell cycle arrest.
ZINC69391 (50 μM; 24 hours) triggers apoptosis on human acute leukemic cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ZINC69391 (25 mg/kg; i.p; daily for 21 days) impairs metastatic lung colonization in a syngeneic animal model. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Specific pathogen-free f
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Cabrera M, et al. Pharmacological Rac1 inhibitors with selective apoptotic activity in human acute leukemic cell lines. Oncotarget. 2017;8(58):98509‐98523. Published 2017 Oct 4.
[2]. Cardama GA, et al. Proapoptotic and antiinvasive activity of Rac1 small molecule inhibitors on malignant glioma cells. Onco Targets Ther. 2014;7:2021‐2033. Published 2014 Oct 30.
溶解度数据
In Vitro: DMSO : 25 mg/mL (80.83 mM; ultrasonic and warming and heat to 60°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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